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SELGANTOLIMOD

SELGANTOLIMOD : Agonist of TLR8

Structure

Information

  • TLR8
  • Agonist
  • up to 1 uM

In Vitro Validations

Uniprot ID: Q9NR97
Target Class: GPCR
Target SubClass: Toll-like receptor
PDB ID for probe-target interaction (3D structure): 6WML
Target aliases:
Toll-like receptor 8, TLR8, TLR8_HUMAN

DOI Reference: 10.1021/acs.jmedchem.0c00100

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): The broader selectivity profile of (R)-7 toward immune receptors was assessed in reporter gene assays using HEK293 cells, stably expressing individual human TLRs or other innate immune receptors. Moreover, (R)-7 did not stimulate HEK293 cells stably expressing other human TLRs including TLR2, TLR3, TLR4, TLR5, TLR9, and other receptors including Nod-like receptors (NLRs: NOD1 and NOD2), RIG-I -like receptors (RLRs; RIG-I and MDA5), or C-type lectin receptors (CLRs; Dectin1a, Dectin 1b, and Mincle).
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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Although there is no direct demonstration of in-cell target engagement and PD biomarkers are quite distal (cytokine and reporter gene endpoints), the lack of activity across a range of related receptors and the structural data supporting the SAR point to a potent and selective TLR8 agonist.

(last updated: 18 Oct 2022 )

SERP Ratings

In Model Organisms

SERP Comments:

Extensive validation supports (R)-7 as a probe with excellent selectivity for TRL8 among the TRL family. Although biophysical characterization is limited, this probe has been well characterized in cells and model organisms for its intended use.

(last updated: 20 Oct 2022 )

SERP+ Ratings

In Cell Rating
In Model Organisms

SERP+ Comments:

The binding mechanism is still unclear as no co-crystal structure or relevant experimental assay has been released.

(last updated: 14 Oct 2025 )